Jun Zhang, Yun Hu, Hai-Yang Wang
Jan 5, 2018
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Journal
Organic Process Research & Development
Abstract
We report a five-step synthesis of 2-cyano-5-formyl-4-methyl-1H-indole through sequential functionalization of readily available 4-methyl-1H-indole. Cyano and aldehyde functionalities are regioselectively installed at the 2 and 5 position, respectively. The sequence is concise and high-yielding, amenable for kilogram scale production.